It is well known that current methods of drug discovery share one critical bottleneck: rediscovery of known, previously identified biological active compounds is prohibitively expensive. This makes the process of discovering novel compounds impractical.
For example, the standard manner in which new antibiotics are discovered involves overlaying a culture of a test strain of bacteria with a culture of a suspected producer of an antibiotic and then observing the culture for zones of inhibition. While this allows for the detection of antimicrobial activity, it does not provide any information as to the chemical nature of the activity leading to the inhibition of growth. Tracing, isolating, and identifying the source molecule of the activity requires then a substantial effort of natural product chemistry. Taking antibiotics as an example, it has been estimated that it may take up to 108 microbial isolates to discover a novel useful antimicrobial.
While growing this number of isolates is feasible, de-replicating the antimicrobial compounds they produce, rediscovering in the process many or all of the antimicrobials so far described is far beyond the capabilities of today's analytical chemistry. As a result, natural product discovery divisions in big pharmaceutical companies have been closed down. In the meantime, the pipeline of novel antibiotics has dried up, and the need for them became urgent and critical.
New drug compounds are currently discovered by overlaying a source of unknown compounds over a test culture and observing the test culture for changes in growth or particular cellular activities. For example, the standard manner in which new antibiotics are discovered involves overlaying a culture of a test strain of bacteria with a culture of a suspected producer of an antibiotic and then observing the culture for zones of inhibition. While this allows for the detection of antimicrobial activity, it does not provide any information as to the chemical nature of the activity leading to the inhibition of growth. Tracing, isolating, and identifying the source molecule of the activity requires then a substantial effort of natural product chemistry. The process is similar for compounds having other desired properties, such as the suppression of growth or killing of cancer cells, and the modulation and manipulation of inflammatory pathways. Thus, discovery of chemically novel compounds having important properties for the treatment of disease causes researchers to rediscover some or all of the known compounds, making this process commercially impractical.
Thus, there remains a need in the art for rapid and efficient methods of screening unknown compounds for antimicrobial, anti-inflammatory, and/or anti-cancer properties. The inventions disclosed herein are likely to dramatically increase the speed of novel compound discovery, radically transforming today's methods of drug discovery.